2-Minute Neuroscience: Naloxone (Narcan)

Описание: Naloxone, also known by the brand name Narcan, is a medication that can be used to treat opioid overdose and substantially reduce the risk of death associated with opioid toxicity. In this video, I discuss the pharmacology of naloxone.

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TRANSCRIPT

Naloxone, also known by the brand name Narcan, is a medication that can be used to treat opioid overdose and substantially reduce the risk of death associated with opioid toxicity. The drug is a competitive antagonist at opioid receptors, which means that it works by binding to the same receptors that opioid drugs bind to, but instead of activating those receptors like opioid drugs, naloxone blocks activity at them. Naloxone also causes opioid drugs that are already attached to the receptor to be displaced. This combination of receptor blockade and removal of active opioid drugs makes naloxone capable of reversing an opioid overdose and reducing the risk of complications associated with one.

Naloxone is commonly administered by injection or nasal spray, but intranasal administration has become a preferred method due to its ease of use and safety. The drug typically begins working within a few minutes, with the exact time to onset being dependent on the route of administration. The effectiveness of naloxone can vary due to a number of factors, including the potency of the opioid in the patient’s system and the dose of opioids they administered. Repeated doses of naloxone are sometimes used to keep the patient from re-experiencing effects of opioids still present in their system after naloxone begins to wear off.

When naloxone is administered to someone with opioids in their system it can cause acute withdrawal symptoms due to the sudden cessation of activity at opioid receptors. While there is some risk associated with complications of acute withdrawal, it is considered low especially compared to the risk of complications linked to opioid overdose. Naloxone administered to someone who has not used opioids recently typically has little to no effect.

REFERENCES

Aziz R, Nguyen L, Ruhani W, Nguyen A, Zachariah B. The Optimal Initial Dose and Route of Naloxone Administration for Successful Opioid Reversal: A Systematic Literature Review. Cureus. 2024 Jan 21;16(1):e52671. doi: 10.7759/cureus.52671. PMID: 38380203; PMCID: PMC10878679.

Rzasa Lynn R, Galinkin JL. Naloxone dosage for opioid reversal: current evidence and clinical implications. Ther Adv Drug Saf. 2018 Jan;9(1):63-88. doi: 10.1177/2042098617744161. Epub 2017 Dec 13. PMID: 29318006; PMCID: PMC5753997.

Saari TI, Strang J, Dale O. Clinical Pharmacokinetics and Pharmacodynamics of Naloxone. Clin Pharmacokinet. 2024 Apr;63(4):397-422. doi: 10.1007/s40262-024-01355-6. Epub 2024 Mar 14. PMID: 38485851; PMCID: PMC11052794.


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